Martin Lee, Wilson Clive G, Koosha Fariba, Tetley Laurence, Gray Alexander I, Senel Sevda, Uchegbu Ijeoma F
Department of Pharmaceutical Sciences, Strathclyde Institute for Biological Sciences, University of Strathclyde, 27 Taylor St., Glasgow G4 0NR, UK.
J Control Release. 2002 Apr 23;80(1-3):87-100. doi: 10.1016/s0168-3659(02)00005-6.
A non-covalently cross-linked palmitoyl glycol chitosan (GCP) hydrogel has been evaluated as an erodible controlled release system for the delivery of hydrophilic macromolecules. Samples of GCP with hydrophobicity decreasing in the order GCP12>GCP11>GCP21 were synthesised and characterised by 1H NMR. Hydrogels were prepared by freeze-drying an aqueous dispersion of the polymer in the presence or absence of either a model macromolecule fluorescein isothiocyanate-dextran (FITC-dextran, MW 4400), and/or amphiphilic derivatives Gelucire 50/13 or vitamin E d-alpha-tocopherol polyethylene glycol succinate. Gels were analysed for aqueous hydration, FITC-dextran release, and bioadhesion, and imaged by scanning electron microscopy. The gels were highly porous and could be hydrated to up to 95x their original weight without an appreciable volume change and most gels eventually eroded. Hydration and erosion were governed by the hydrophobicity of the gel and the presence of the amphiphilic additives. GCP gels could be loaded with up to 27.5% (w/w) of FITC-dextran by freeze-drying a dispersion of GCP in a solution of FITC-dextran. The controlled release of FITC-dextran was governed by the hydrophobicity of the gel following the trend GCP21>GCP11>GCP12. GCP gels were bioadhesive but less so than hydroxypropylmethylcellulose, Carbopol 974NF (7:3) tablets.
一种非共价交联的棕榈酰化壳聚糖(GCP)水凝胶已被评估为一种可侵蚀的控释系统,用于亲水性大分子的递送。合成了疏水性按GCP12>GCP11>GCP21顺序降低的GCP样品,并通过1H NMR进行了表征。通过在存在或不存在模型大分子异硫氰酸荧光素-葡聚糖(FITC-葡聚糖,分子量4400)和/或两亲性衍生物Gelucire 50/13或维生素E d-α-生育酚聚乙二醇琥珀酸酯的情况下冻干聚合物的水分散体来制备水凝胶。对凝胶进行了水合作用、FITC-葡聚糖释放和生物粘附分析,并通过扫描电子显微镜成像。凝胶具有高度多孔性,可以水合至其原始重量的95倍而体积没有明显变化,并且大多数凝胶最终会被侵蚀。水合作用和侵蚀作用受凝胶的疏水性和两亲性添加剂的存在影响。通过冻干GCP在FITC-葡聚糖溶液中的分散体,GCP凝胶可以负载高达27.5%(w/w)的FITC-葡聚糖。FITC-葡聚糖的控释受凝胶疏水性的控制,遵循GCP21>GCP11>GCP12的趋势。GCP凝胶具有生物粘附性,但比羟丙基甲基纤维素、卡波姆974NF(7:3)片剂的生物粘附性要低。